DGIdb - TOLBUTAMIDE Drug Record

TOLBUTAMIDE chembl:CHEMBL782 Approved

Alternate Names:

NSC-87833
RASTINON
GLYCONON
PRAMIDEX
TOLBUTAMIDE
ORINASE
NSC-23813
N-(SULFONYL-P-METHYLBENZENE)-N'-N-BUTYLUREA
1-BUTYL-3-(P-METHYLPHENYLSULFONYL)UREA
1-BUTYL-3-(P-TOLYLSULFONYL)UREA
3-(P-TOLYL-4-SULFONYL)-1-BUTYLUREA
N-(P-METHYLBENZENESULFONYL)-N'-BUTYLUREA
N-N-BUTYL-N'-TOSYLUREA
1-P-TOLUENESULFONYL-3-BUTYLUREA
N-BUTYL-N'-P-TOLUENESULFONYLUREA
1-BUTYL-3-TOSYLUREA
N-(4-METHYLBENZENESULFONYL)-N'-BUTYLUREA
N-BUTYL-N'-(4-METHYLPHENYLSULFONYL)UREA
ORINASE (TN)
N-BUTYL-N'-(P-TOLYLSULFONYL)UREA
TOLBUTAMIDUM
TOLYLSULFONYLBUTYLUREA
TOLBUTAMIDA
N-(4-METHYLPHENYLSULFONYL)-N'-BUTYLUREA
TOLBUTAMIDE SODIUM
ORINASE®
chembl:CHEMBL782
drugbank:01124
pubchem.compound:5505
chemidplus:64-77-7
rxcui:10635

Drug Info:

Year of Approval	approved before 1982
Drug Class	hypoglycemic agents
Drug Categories	tests for diabetes
Drug Categories	sulfur compounds
FDA Approval	Approved before 1982
Drug Class	small molecule
Drug Indications	Hypoglycemic Agents
Drug Groups	investigational
Drug Categories	alimentary tract and metabolism
Drug Categories	cytochrome p-450 cyp2c18 substrates
Drug Categories	cytochrome p-450 cyp2c8 inhibitors (strength unknown)
Drug Categories	cytochrome p-450 enzyme inhibitors
Drug Categories	cytochrome p-450 substrates
Drug Categories	drugs that are mainly renally excreted
Drug Categories	drugs used in diabetes
Drug Categories	oat1/slc22a6 inhibitors
Drug Categories	sulfonylureas

(5 More Sources)

Publications:

Mizuno et al., 2008, Type 2 diabetes and oral antihyperglycemic drugs., Curr. Med. Chem.
Liu et al., 1999, ATP-dependent activation of K(Ca) and ROMK-type K(ATP) channels in human submandibular gland ductal cells., J. Biol. Chem.
Smith et al., 1998, Inhibition of the ATP-sensitive potassium channel from mouse pancreatic beta-cells by surfactants., Br. J. Pharmacol.
Proks et al., 2001, Interaction of stilbene disulphonates with cloned K(ATP) channels., Br. J. Pharmacol.
Blaisdell J et al., 2004, Discovery of new potentially defective alleles of human CYP2C9., Pharmacogenetics
Jones BC et al., 1996, Putative active site template model for cytochrome P4502C9 (tolbutamide hydroxylase)., Drug Metab Dispos
Kirchheiner J et al., 2002, Impact of CYP2C9 and CYP2C19 polymorphisms on tolbutamide kinetics and the insulin and glucose response in healthy volunteers., Pharmacogenetics
Dai DP et al., 2015, Identification and Functional Assessment of a New CYP2C9 Allelic Variant CYP2C9*59., Drug Metab Dispos
Gao N et al., 2016, Gene polymorphisms and contents of cytochrome P450s have only limited effects on metabolic activities in human liver microsomes., Eur J Pharm Sci
Chen H et al., 2020, An identification and functional evaluation of a novel CYP2C9 variant CYP2C9*62., Chem Biol Interact
Ibeanu GC et al., 1998, An additional defective allele, CYP2C19*5, contributes to the S-mephenytoin poor metabolizer phenotype in Caucasians., Pharmacogenetics
Ibeanu GC et al., 1999, A novel transversion in the intron 5 donor splice junction of CYP2C19 and a sequence polymorphism in exon 3 contribute to the poor metabolizer phenotype for the anticonvulsant drug S-mephenytoin., J Pharmacol Exp Ther

TOLBUTAMIDE KCNJ1

Interaction Score: 2.37

Interaction Types & Directionality:

inhibitor (inhibitory)

Interaction Info:

Trial Name -

Novel drug target Established target

PMIDs:
10455193 9647478 11226127

Sources:
TEND TdgClinicalTrial DrugBank
TOLBUTAMIDE ABCC8

Interaction Score: 1.49

Interaction Types & Directionality:

blocker (inhibitory)

inhibitor (inhibitory)

Interaction Info:

Mechanism of Interaction Sulfonylurea receptor 1, Kir6.2 blocker

Direct Interaction yes

PMIDs:
18220763

Sources:
TTD DrugBank ChemblInteractions
TOLBUTAMIDE ABCC9

Interaction Score: 0.65

Interaction Types & Directionality:

n/a

Interaction Info:

PMIDs:
None found

Sources:
TTD
TOLBUTAMIDE KCNJ8

Interaction Score: 0.59

Interaction Types & Directionality:

inhibitor (inhibitory)

Interaction Info:

Direct Interaction? False

Endogenous Drug? False

Specific Action of the Ligand None

PMIDs:
None found

Sources:
GuideToPharmacology
TOLBUTAMIDE KCNJ11

Interaction Score: 0.44

Interaction Types & Directionality:

blocker (inhibitory)

inhibitor (inhibitory)

Interaction Info:

Mechanism of Interaction Sulfonylurea receptor 1, Kir6.2 blocker

Direct Interaction yes

Specific Action of the Ligand None

PMIDs:
None found

Sources:
GuideToPharmacology ChemblInteractions
TOLBUTAMIDE G6PD

Interaction Score: 0.19

Interaction Types & Directionality:

n/a

Interaction Info:

PMIDs:
None found

Sources:
FDA PharmGKB
TOLBUTAMIDE CYP2C9

Interaction Score: 0.12

Interaction Types & Directionality:

n/a

Interaction Info:

PMIDs:
15284535 8742240 11875364 25994031 27339126 32531309

Sources:
PharmGKB
TOLBUTAMIDE CYP2C19

Interaction Score: 0.05

Interaction Types & Directionality:

n/a

Interaction Info:

PMIDs:
10022751 10411572

Sources:
PharmGKB

DrugBank: DB01124

Version: 5.1.7

Alternate Names:

Orinase 1gm Drug Brand

Rastinon Drug Brand

Tolbutamide Drug Brand

Drug Info:

Drug Type small molecule

Drug Groups approved

Drug Groups investigational

Publications:

Mizuno et al., 2008, Type 2 diabetes and oral antihyperglycemic drugs., Curr. Med. Chem.

Liu et al., 1999, ATP-dependent activation of K(Ca) and ROMK-type K(ATP) channels in human submandibular gland ductal cells., J. Biol. Chem.

Smith et al., 1998, Inhibition of the ATP-sensitive potassium channel from mouse pancreatic beta-cells by surfactants., Br. J. Pharmacol.

TEND: TOLBUTAMIDE
- Version: 01-August-2011
Alternate Names:

TOLBUTAMIDE Primary Drug Name

Drug Info:

Drug Class hypoglycemic agents

Year of Approval approved before 1982

Publications:
TdgClinicalTrial: TOLBUTAMIDE
- Version: January-2014
Alternate Names:

Drug Info:

Drug Indications Hypoglycemic Agents

Drug Class small molecule

FDA Approval Approved before 1982

Publications:

PharmGKB: tolbutamide

Version: 18-August-2020

Alternate Names:

Drug Info:

Publications:

Blaisdell J et al., 2004, Discovery of new potentially defective alleles of human CYP2C9., Pharmacogenetics

Jones BC et al., 1996, Putative active site template model for cytochrome P4502C9 (tolbutamide hydroxylase)., Drug Metab Dispos

Kirchheiner J et al., 2002, Impact of CYP2C9 and CYP2C19 polymorphisms on tolbutamide kinetics and the insulin and glucose response in healthy volunteers., Pharmacogenetics

TTD: Tolbutamide
- Version: 2020.06.01
Alternate Names:

D06OIV TTD Drug ID

Drug Info:

Publications:
GuideToPharmacology: 178103454
- Version: 29-September-2020
Alternate Names:

TOLBUTAMIDE GuideToPharmacology Ligand Name

Drug Info:

Publications:
ChemblInteractions: CHEMBL782
- Version: chembl_23
Alternate Names:

Drug Info:

Publications:
ChemblDrugs: chembl:CHEMBL782
- Version: ChEMBL_27
Alternate Names:

Drug Info:

Publications:
FDA: Tolbutamide
- Version: 04-September-2020
Alternate Names:

Drug Info:

Publications:

Mechanism of Interaction	Sulfonylurea receptor 1, Kir6.2 blocker
Direct Interaction	yes

Direct Interaction?	False
Endogenous Drug?	False
Specific Action of the Ligand	None

Orinase 1gm	Drug Brand
Rastinon	Drug Brand
Tolbutamide	Drug Brand

Drug Type	small molecule
Drug Groups	approved
Drug Groups	investigational

Trial Name	-
Novel drug target	Established target

blocker (inhibitory)
inhibitor (inhibitory)

blocker (inhibitory)
inhibitor (inhibitory)

TOLBUTAMIDE Drug Record

TOLBUTAMIDE chembl:CHEMBL782 Approved

Alternate Names:

Drug Info:

Publications:

Interaction Types & Directionality: inhibitor (inhibitory)

Interaction Info: Trial Name - Novel drug target Established target

PMIDs: 10455193 9647478 11226127

Sources: TEND TdgClinicalTrial DrugBank

Interaction Types & Directionality: blocker (inhibitory) inhibitor (inhibitory)

Interaction Info: Mechanism of Interaction Sulfonylurea receptor 1, Kir6.2 blocker Direct Interaction yes

PMIDs: 18220763

Sources: TTD DrugBank ChemblInteractions

Interaction Types & Directionality: n/a

Interaction Info:

PMIDs: None found

Sources: TTD

Interaction Types & Directionality: inhibitor (inhibitory)

Interaction Info: Direct Interaction? False Endogenous Drug? False Specific Action of the Ligand None

PMIDs: None found

Sources: GuideToPharmacology

Interaction Types & Directionality: blocker (inhibitory) inhibitor (inhibitory)

Interaction Info: Mechanism of Interaction Sulfonylurea receptor 1, Kir6.2 blocker Direct Interaction yes Specific Action of the Ligand None

PMIDs: None found

Sources: GuideToPharmacology ChemblInteractions

Interaction Types & Directionality: n/a

Interaction Info:

PMIDs: None found

Sources: FDA PharmGKB

Interaction Types & Directionality: n/a

Interaction Info:

PMIDs: 15284535 8742240 11875364 25994031 27339126 32531309

Sources: PharmGKB

Interaction Types & Directionality: n/a

Interaction Info:

PMIDs: 10022751 10411572

Sources: PharmGKB

DrugBank: DB01124

Alternate Names: Orinase 1gm Drug Brand Rastinon Drug Brand Tolbutamide Drug Brand

Drug Info: Drug Type small molecule Drug Groups approved Drug Groups investigational

TEND: TOLBUTAMIDE

Alternate Names: TOLBUTAMIDE Primary Drug Name

Drug Info: Drug Class hypoglycemic agents Year of Approval approved before 1982

Publications:

TdgClinicalTrial: TOLBUTAMIDE

Alternate Names:

Drug Info: Drug Indications Hypoglycemic Agents Drug Class small molecule FDA Approval Approved before 1982

Publications:

PharmGKB: tolbutamide

Alternate Names:

Drug Info:

TTD: Tolbutamide

Alternate Names: D06OIV TTD Drug ID

Drug Info:

Publications:

GuideToPharmacology: 178103454

Alternate Names: TOLBUTAMIDE GuideToPharmacology Ligand Name

Drug Info:

Publications:

ChemblInteractions: CHEMBL782

Alternate Names:

Drug Info:

Publications:

ChemblDrugs: chembl:CHEMBL782

Alternate Names:

Drug Info:

Publications:

FDA: Tolbutamide

Alternate Names:

Drug Info:

Publications:

Interaction Types & Directionality:

inhibitor (inhibitory)

Interaction Info:

Trial Name -

Novel drug target Established target

PMIDs:
10455193 9647478 11226127

Sources:
TEND TdgClinicalTrial DrugBank

Interaction Types & Directionality:

blocker (inhibitory)

inhibitor (inhibitory)

Interaction Info:

Mechanism of Interaction Sulfonylurea receptor 1, Kir6.2 blocker

Direct Interaction yes

PMIDs:
18220763

Sources:
TTD DrugBank ChemblInteractions

Interaction Types & Directionality:

n/a

PMIDs:
None found

Sources:
TTD

Interaction Types & Directionality:

inhibitor (inhibitory)

Interaction Info:

Direct Interaction? False

Endogenous Drug? False

Specific Action of the Ligand None

PMIDs:
None found

Sources:
GuideToPharmacology

Interaction Types & Directionality:

blocker (inhibitory)

inhibitor (inhibitory)

Interaction Info:

Mechanism of Interaction Sulfonylurea receptor 1, Kir6.2 blocker

Direct Interaction yes

Specific Action of the Ligand None

PMIDs:
None found

Sources:
GuideToPharmacology ChemblInteractions

Interaction Types & Directionality:

n/a

PMIDs:
None found

Sources:
FDA PharmGKB

Interaction Types & Directionality:

n/a

PMIDs:
15284535 8742240 11875364 25994031 27339126 32531309

Sources:
PharmGKB

Interaction Types & Directionality:

n/a

PMIDs:
10022751 10411572

Sources:
PharmGKB

Alternate Names:

Orinase 1gm Drug Brand

Rastinon Drug Brand

Tolbutamide Drug Brand

Drug Info:

Drug Type small molecule

Drug Groups approved

Drug Groups investigational

Alternate Names:

TOLBUTAMIDE Primary Drug Name

Drug Info:

Drug Class hypoglycemic agents

Year of Approval approved before 1982

Drug Info:

Drug Indications Hypoglycemic Agents

Drug Class small molecule

FDA Approval Approved before 1982

Alternate Names:

D06OIV TTD Drug ID

Alternate Names:

TOLBUTAMIDE GuideToPharmacology Ligand Name